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首页> 外文期刊>Parasitology Research >Anthelmintic activity of Artemisia annua L. extracts in vitro and the effect of an aqueous extract and artemisinin in sheep naturally infected with gastrointestinal nematodes
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Anthelmintic activity of Artemisia annua L. extracts in vitro and the effect of an aqueous extract and artemisinin in sheep naturally infected with gastrointestinal nematodes

机译：青蒿提取物的体外驱虫活性以及水提取物和青蒿素对天然感染胃肠道线虫的绵羊的影响

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摘要

There is no effective natural alternative control for gastrointestinal nematodes (GIN) of small ruminants, with Haemonchus contortus being the most economically important GIN. Despite frequent reports of multidrug-resistant GIN, there is no new commercial anthelmintic to substitute failing ones. Although trematocidal activity of artemisinin analogs has been reported in sheep, neither artemisinin nor its plant source (Artemisia annua) has been evaluated for anthelmintic activity in ruminants. This study evaluated the anthelmintic activity of A. annua crude extracts in vitro and compared the most effective extract with artemisinin in sheep naturally infected with H. contortus. A. annua leaves extracted with water, aqueous 0.1 % sodium bicarbonate, dichloromethane, and ethanol were evaluated in vitro by the egg hatch test (EHT) and with the bicarbonate extract only for the larval development test (LDT) using H. contortus. The A. annua water, sodium bicarbonate (SBE), ethanol, and dichloromethane extracts tested in vitro contained 0.3, 0.6, 4.4, and 9.8 % of artemisinin, respectively. The sodium bicarbonate extract resulted in the lowest LC99 in the EHT (1.27 μg/mL) and in a LC99 of 23.8 μg/mL in the LDT. Following in vitro results, the SBE (2 g/kg body weight (BW)) and artemisinin (100 mg/kg BW) were evaluated as a single oral dose in naturally infected Santa Inês sheep. Speciation from stool cultures established that 84-91 % of GIN were H. contortus, 8.4-15.6 % were Trichostrongylus sp., and 0.3-0.7 % were Oesophagostomum sp. Packed-cell volume and eggs per gram (EPG) of feces were used to test treatment efficacy. The SBE tested in vivo contained no artemisinin, but had a high antioxidant capacity of 2,295 μmol of Trolox equivalents/g. Sheep dosed with artemisinin had maximum feces concentrations 24 h after treatment (126.5 μg/g artemisinin), which sharply decreased at 36 h. By day 15, only levamisole-treated sheep had a significant decrease of 97 % in EPG. Artemisinin-treated and SBE-treated sheep had nonsignificant EPG reductions of 28 and 19 %, respectively, while sheep in infected/untreated group had an average EPG increase of 95 %. Sheep treated with artemisinin and A. annua SBE maintained blood hematocrits throughout the experiment, while untreated/infected controls had a significant reduction in hematocrit. This is the first time oral dose of artemisinin and an aqueous extract of A. annua are evaluated as anthelmintic in sheep. Although oral dose of artemisinin and SBE, at single doses, were ineffective natural anthelmintics, artemisinin analogs with better bioavailability than artemisinin should be tested in vivo, through different routes and in multiple doses. The maintenance of hematocrit provided by artemisinin and A. annua extract and the high antioxidant capacity of the latter suggest that they could be combined with commercial anthelmintics to improve the well-being of infected animals and to evaluate potential synergism.
机译：小型反刍动物的胃肠道线虫（GIN）没有有效的自然替代控制方法，而捻转血矛线虫（Haemonchus contortus）是最经济的GIN。尽管关于耐多药GIN的报道屡见不鲜，但尚无新的商业驱虫药来替代失败的GIN。尽管在绵羊中已报道了青蒿素类似物的杀真菌活性，但尚未对青蒿素或其植物来源（青蒿）的反刍动物驱虫活性进行评估。这项研究评估了在体外被天然感染H. contortus的绵羊中的A. annua粗提取物的驱虫活性，并将最有效的提取物与青蒿素进行了比较。用水，0.1％碳酸氢钠水溶液，二氯甲烷和乙醇提取的桔梗叶片在体外通过卵孵化试验（EHT）进行了评估，仅用碳酸氢盐提取物进行了阔叶幼虫的幼体发育测试（LDT）。体外测试的青蒿水，碳酸氢钠（SBE），乙醇和二氯甲烷提取物分别含有0.3％，0.6％，4.4％和9.8％的青蒿素。碳酸氢钠提取物在EHT中的LC99最低（1.27μg/ mL），在LDT中的LC99最低为23.8μg/ mL。在体外结果之后，将SBE（2 g / kg体重（BW））和青蒿素（100 mg / kg BW）作为单次口服剂量评估为自然感染的SantaInês绵羊。从粪便培养物的种类确定，GIN的84-91％为Contortus，曲毛虫为8.4-15.6％，食管食管菌为0.3-0.7％。填充细胞体积和每克粪便中的鸡蛋数（EPG）用于测试治疗效果。体内测试的SBE不包含青蒿素，但具有2,295μmolTrolox当量/ g的高抗氧化能力。给予青蒿素的绵羊在治疗后24小时的最大粪便浓度为（126.5μg/ g青蒿素），在36小时时急剧下降。到第15天，仅用左旋咪唑治疗的绵羊的EPG显着降低了97％。青蒿素处理的绵羊和SBE处理的绵羊的EPG分别降低了28％和19％，而感染/未治疗组的绵羊的EPG平均增加了95％。在整个实验过程中，用青蒿素和A.annua SBE处理的绵羊维持血细胞比容，而未处理/感染的对照的血细胞比容显着降低。这是青蒿素和青蒿的水提取物的口服剂量首次被评估为绵羊驱虫药。尽管口服青蒿素和SBE的单次剂量是无效的天然驱虫药，但应通过不同途径和多次剂量在体内测试具有比青蒿素更好的生物利用度的青蒿素类似物。青蒿素和青蒿提取物提供的血细胞比容维持能力和后者的高抗氧化能力表明，它们可以与商业驱虫药结合使用，以改善感染动物的健康并评估潜在的协同作用。

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